发明授权
- 专利标题: Cinnamide derivatives as KCNQ potassium channel modulators
- 专利标题(中): 桂酰胺衍生物作为KCNQ钾通道调节剂
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申请号: US10160582申请日: 2002-05-31
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公开(公告)号: US06831080B2公开(公告)日: 2004-12-14
- 发明人: Yong-Jin Wu , Li-Quang Sun , Jie Chen , Huan He , Alexandre L'Heureux , Pierre Dextraze , Jean-Paul Daris , Gene G. Kinney , Steven I. Dworetzky , Piyasena Hewawasam
- 申请人: Yong-Jin Wu , Li-Quang Sun , Jie Chen , Huan He , Alexandre L'Heureux , Pierre Dextraze , Jean-Paul Daris , Gene G. Kinney , Steven I. Dworetzky , Piyasena Hewawasam
- 主分类号: C07C23720
- IPC分类号: C07C23720
摘要:
There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken together are —CH═CH—CH═CH— or —X(CH2)mY— in which X and Y are each independently selected from the group consisting of CH2, (CH2)nN(R9)— and O, wherein m is 1 or 2; n is 0 or 1; and R6, R7, and R8 are each independently selected from hydrogen, chloro and fluoro; and R9 is selected from the group consisting of hydrogen, C1-4 alkyl, hydroxyethyl, C1-4 alkoxyethyl, cyclopropylmethyl, —CO2(C1-4alkyl), and —CH2CH2NR10R11 in which R10 and R11 are each independently hydrogen or C1-4 alkyl, which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.
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